JP2009501746A5 - - Google Patents

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JP2009501746A5
JP2009501746A5 JP2008521876A JP2008521876A JP2009501746A5 JP 2009501746 A5 JP2009501746 A5 JP 2009501746A5 JP 2008521876 A JP2008521876 A JP 2008521876A JP 2008521876 A JP2008521876 A JP 2008521876A JP 2009501746 A5 JP2009501746 A5 JP 2009501746A5
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Prior art keywords
amino
ethyl
purin
trans
imidazol
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JP2008521876A
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JP5010599B2 (en
JP2009501746A (en
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Priority claimed from GBGB0514809.3A external-priority patent/GB0514809D0/en
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Claims (9)

式(I)：
Figure 2009501746
 [式中、
R1は、メチルまたはエチルを表し；
R2は、下記のリスト：
Figure 2009501746
 より選択される基を表し；
R3は、下記のリスト：
Figure 2009501746
 より選択される基を表し；
ここで、R4は、下記のリスト：
Figure 2009501746
 より選択される基を表し；
R5は、水素、C1-4アルキル、C1-4アルキルアリール、C1-4アルキルヘテロアリールまたはC1-4ヒドロキシアルキルを表し；
R6およびR7は独立して、水素、メチルまたはフェニルを表す]
の化合物、ならびにその塩および溶媒和物。 Formula (I):
Figure 2009501746
 [Where
R 1 represents methyl or ethyl;
R 2 has the following list:
Figure 2009501746
 Represents a group selected from;
R 3 lists below:
Figure 2009501746
 Represents a group selected from;
Where R 4 is the list below:
Figure 2009501746
 Represents a group selected from;
R 5 represents hydrogen, C 1-4 alkyl, C 1-4 alkylaryl, C 1-4 alkylheteroaryl or C 1-4 hydroxyalkyl;
R 6 and R 7 independently represent hydrogen, methyl or phenyl]
And their salts and solvates. R1がエチルを表す、請求項1に記載の化合物。 2. A compound according to claim 1, wherein R < 1 > represents ethyl. R2が基(i)、(ii)、(iii)または(iv)を表す、請求項1または請求項2に記載の化合物。 3. A compound according to claim 1 or claim 2, wherein R2 represents a group (i), (ii), (iii) or (iv). R5がHを表す、請求項1〜3のいずれか1項に記載の化合物。 R 5 represents H, compound according to any one of claims 1 to 3. R4が基(i)、(ii)、(iii)、(iv)または(v)を表す、請求項1〜4のいずれか1項に記載の化合物。 R 4 is a group (i), (ii), (iii), (iv) or (v) represents a compound according to any one of claims 1 to 4. (2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[2-(1H-イミダゾール-4-イル)エチル]アミノ}-6-({trans-4-[(2-{[2-(1H-イミダゾール-4-イル)エチル]アミノ}-1H-プリン-6-イル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[2-(1-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-6-({trans-4-[(2-{[2-(1-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-1H-プリン-6-イル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[2-(5-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-6-({trans-4-[(2-{[2-(5-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-1H-プリン-6-イル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[4-(1-ピロリジニル)ブチル]アミノ}-6-({trans-4-[(2-{[4-(1-ピロリジニル)ブチル]アミノ}-1H-プリン-6-イル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3R,4S,5R)-2-(2-[(trans-4-アミノシクロヘキシル)アミノ]-6-{[trans-4-({2-[(trans-4-アミノシクロヘキシル)アミノ]-9H-プリン-6-イル}アミノ)シクロヘキシル]アミノ}-9H-プリン-9-イル)-5-(2-エチル-2H-テトラゾール-5-イル)テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[2-(1H-イミダゾール-4-イル)エチル]アミノ}-6-({trans-4-[(2-{[2-(1H-イミダゾール-4-イル)エチル]アミノ}-4-ピリミジニル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[2-(1-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-6-({trans-4-[(2-{[2-(1-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-4-ピリミジニル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[2-(5-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-6-({trans-4-[(2-{[2-(5-メチル-1H-イミダゾール-4-イル)エチル]アミノ}-4-ピリミジニル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3S,4R,5R)-2-(2-エチル-2H-テトラゾール-5-イル)-5-[2-{[4-(1-ピロリジニル)ブチル]アミノ}-6-({trans-4-[(2-{[4-(1-ピロリジニル)ブチル]アミノ}-4-ピリミジニル)アミノ]シクロヘキシル}アミノ)-9H-プリン-9-イル]テトラヒドロ-3,4-フランジオール；
(2R,3R,4S,5R)-2-(2-[(trans-4-アミノシクロヘキシル)アミノ]-6-{[trans-4-({2-[(trans-4-アミノシクロヘキシル)アミノ]-4-ピリミジニル}アミノ)シクロヘキシル]アミノ}-9H-プリン-9-イル)-5-(2-エチル-2H-テトラゾール-5-イル)テトラヒドロ-3,4-フランジオール；
である式(I)の化合物、またはそれらのいずれか1つの塩もしくは溶媒和物。 (2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[2- (1H-imidazol-4-yl) ethyl] amino} -6 -({trans-4-[(2-{[2- (1H-imidazol-4-yl) ethyl] amino} -1H-purin-6-yl) amino] cyclohexyl} amino) -9H-purine-9- Yl] tetrahydro-3,4-furandol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[2- (1-methyl-1H-imidazol-4-yl) ethyl] Amino} -6-({trans-4-[(2-{[2- (1-methyl-1H-imidazol-4-yl) ethyl] amino} -1H-purin-6-yl) amino] cyclohexyl} amino ) -9H-purin-9-yl] tetrahydro-3,4-furandol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[2- (5-methyl-1H-imidazol-4-yl) ethyl] Amino} -6-({trans-4-[(2-{[2- (5-methyl-1H-imidazol-4-yl) ethyl] amino} -1H-purin-6-yl) amino] cyclohexyl} amino ) -9H-purin-9-yl] tetrahydro-3,4-furandol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[4- (1-pyrrolidinyl) butyl] amino} -6-({trans -4-[(2-{[4- (1-pyrrolidinyl) butyl] amino} -1H-purin-6-yl) amino] cyclohexyl} amino) -9H-purin-9-yl] tetrahydro-3,4- Flange all;
(2R, 3R, 4S, 5R) -2- (2-[(trans-4-aminocyclohexyl) amino] -6-{[trans-4-({2-[(trans-4-aminocyclohexyl) amino] -9H-purin-6-yl} amino) cyclohexyl] amino} -9H-purin-9-yl) -5- (2-ethyl-2H-tetrazol-5-yl) tetrahydro-3,4-furandol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[2- (1H-imidazol-4-yl) ethyl] amino} -6 -({trans-4-[(2-{[2- (1H-imidazol-4-yl) ethyl] amino} -4-pyrimidinyl) amino] cyclohexyl} amino) -9H-purin-9-yl] tetrahydro- 3,4-flangeol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[2- (1-methyl-1H-imidazol-4-yl) ethyl] Amino} -6-({trans-4-[(2-{[2- (1-methyl-1H-imidazol-4-yl) ethyl] amino} -4-pyrimidinyl) amino] cyclohexyl} amino) -9H- Purin-9-yl] tetrahydro-3,4-furandol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[2- (5-methyl-1H-imidazol-4-yl) ethyl] Amino} -6-({trans-4-[(2-{[2- (5-methyl-1H-imidazol-4-yl) ethyl] amino} -4-pyrimidinyl) amino] cyclohexyl} amino) -9H- Purin-9-yl] tetrahydro-3,4-furandol;
(2R, 3S, 4R, 5R) -2- (2-Ethyl-2H-tetrazol-5-yl) -5- [2-{[4- (1-pyrrolidinyl) butyl] amino} -6-({trans -4-[(2-{[4- (1-pyrrolidinyl) butyl] amino} -4-pyrimidinyl) amino] cyclohexyl} amino) -9H-purin-9-yl] tetrahydro-3,4-furandol;
(2R, 3R, 4S, 5R) -2- (2-[(trans-4-aminocyclohexyl) amino] -6-{[trans-4-({2-[(trans-4-aminocyclohexyl) amino] -4-pyrimidinyl} amino) cyclohexyl] amino} -9H-purin-9-yl) -5- (2-ethyl-2H-tetrazol-5-yl) tetrahydro-3,4-furandol;
Or a salt or solvate of any one of them. 請求項1〜6のいずれか1項に記載の式(I)の化合物を含み、さらに1種以上の製薬上許容される希釈剤または担体を含む医薬組成物。   A pharmaceutical composition comprising a compound of formula (I) according to any one of claims 1 to 6 and further comprising one or more pharmaceutically acceptable diluents or carriers. 医薬品として使用するための請求項1〜6のいずれか1項に記載の化合物。   7. A compound according to any one of claims 1 to 6 for use as a medicament. 炎症性疾患の治療のための医薬品の製造における請求項1〜6のいずれか1項に記載の化合物の使用。   Use of a compound according to any one of claims 1 to 6 in the manufacture of a medicament for the treatment of inflammatory diseases.
JP2008521876A 2005-07-19 2006-07-17 Purine derivatives that are agonists of adenosine A2A receptors Expired - Fee Related JP5010599B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0514809.3A GB0514809D0 (en) 2005-07-19 2005-07-19 Compounds
GB0514809.3 2005-07-19
PCT/EP2006/007078 WO2007009757A1 (en) 2005-07-19 2006-07-17 Purine derivatives as agonists of the adenosine a2a receptor

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JP2009501746A JP2009501746A (en) 2009-01-22
JP2009501746A5 true JP2009501746A5 (en) 2009-08-27
JP5010599B2 JP5010599B2 (en) 2012-08-29

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EP (1) EP1904512B1 (en)
JP (1) JP5010599B2 (en)
AR (1) AR054559A1 (en)
ES (1) ES2387404T3 (en)
GB (1) GB0514809D0 (en)
PE (1) PE20070179A1 (en)
TW (1) TW200740814A (en)
WO (1) WO2007009757A1 (en)

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